Zafar Nadiah, Mahmood Asif, Sarfraz Rai Muhammad, Elaissari Abdelhamid
Faculty of Pharmacy, The University Lahore, Lahore 54000, Pakistan.
Department of Pharmacy, The University of Chakwal, Chakwal 48800, Pakistan.
Micromachines (Basel). 2022 Aug 12;13(8):1304. doi: 10.3390/mi13081304.
Microneedle patches (MNPs) are one of the emerging approaches for drug delivery involving minimal invasion and improved skin penetration of macro- and micro-entities. Herein, we report dissolvable microneedle patches (dMNPs) as a novel tool for better systemic delivery of Simvastatin in the management of hypocholesteremia. Thiolated chitosan (TC), polyvinyl pyrolidone (PVP) and polyvinyl alcohol (PVA) were employed in the development of dMNPs. Developed patches were characterized through SEM, FTIR, DSC, TGA, PXRD, dissolution testing, tensile strength, elongation (%), skin irritation studies, moisture content and pharmacokinetic evaluation. dMNP F26 exhibited excellent tensile strength (9.85 MPa), penetration potential (~700 µm), moisture content (5.95%), elongation (35.54%) and Simvastatin release of 77.92%. Pharmacokinetic properties were also improved, i.e., C 1.97 µg/mL, t 9 h, MRT 19.9 h and AUC 46.24 µg·h/mL as compared to Simvastatin solution displaying C 2.55 µg/mL, t 3 h, MRT 5.91 h and AUC 14.20 µg·h/mL thus confirming higher and improved bioavailability. Kinetic modelling revealed zero order as the best fit model based on regression coefficient. Histopathological findings proved the biocompatibility of the developed dMNPs.
微针贴片(MNPs)是一种新兴的药物递送方法,涉及最小程度的侵入,并能改善大分子和小分子实体的皮肤渗透。在此,我们报告可溶解微针贴片(dMNPs)是一种用于更好地全身递送辛伐他汀以治疗低胆固醇血症的新型工具。在dMNPs的研发中使用了巯基化壳聚糖(TC)、聚乙烯吡咯烷酮(PVP)和聚乙烯醇(PVA)。通过扫描电子显微镜(SEM)、傅里叶变换红外光谱(FTIR)、差示扫描量热法(DSC)、热重分析(TGA)、粉末X射线衍射(PXRD)、溶出度测试、拉伸强度、伸长率(%)、皮肤刺激性研究、水分含量和药代动力学评估对所研发的贴片进行了表征。dMNP F26表现出优异的拉伸强度(9.85兆帕)、渗透潜力(约700微米)、水分含量(5.95%)、伸长率(35.54%)以及77.92%的辛伐他汀释放率。药代动力学性质也得到了改善,即与辛伐他汀溶液相比,dMNP F26的血药浓度峰值(Cmax)为1.97微克/毫升、达峰时间(tmax)为9小时、平均驻留时间(MRT)为19.9小时、药时曲线下面积(AUC)为46.24微克·小时/毫升,而辛伐他汀溶液的Cmax为2.55微克/毫升、tmax为3小时、MRT为5.91小时、AUC为14.20微克·小时/毫升,从而证实了更高且改善的生物利用度。动力学建模表明基于回归系数零级模型为最佳拟合模型。组织病理学结果证明了所研发的dMNPs的生物相容性。